JPH07277988A - Locally itch-removing and treating agent - Google Patents

Abstract

PURPOSE:To prepare a locally itch-removing and treating agent useful for treating skin itches appearing on diabetes and hepatopathy and senile itches much appearing on aged men by locally applying a phosphoric acid diester compound in a constant concentration. CONSTITUTION:The locally itch-removing or treating agent contains a phosphoric acid diester compound of the formula (R1 and R2 are H, methyl) or its pharmacologically acceptable salt so as to contact with an itch-generated site in a concentration of 0.01-5(W/W)%, and is preferably prepared in the formulation of ointments, aqueous solutions or spraying agents. The compound of the formula is e.g. DL-alpha-tocopherol phosphoric acid diester potassium salt. As the concentration of the compound of the formula or its salt contained in the various kinds of formulations, the concentration in an ointment or cream is 0.015(W/W)%, preferably 0.05-2(W/W)%, and the concentration in an aqueous spraying agent is 0.01-5(W/W)%, preferably 0.05-2(W/W)%.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to an agent for removing or treating pruritus. More specifically, the present invention provides the following formula [1]:

[0002]

[Chemical 2] (In the formula, R ₁ and R ₂ are the same or different and each represents a hydrogen atom or a methyl group.) The present invention relates to a pruritus-removing or therapeutic agent containing a phosphodiester compound or a salt thereof.

[0003]

2. Description of the Related Art Conventionally, ammonia water, menthol, camphor, etc. have been used for insect bites, and antihistamines or steroids have been used for the prevention of itch in urticaria. However, since these antipruritic effects are temporary, in many cases, it is necessary not only to continuously use them, but also for steroids, long-term administration requires caution due to side effect problems. Therefore, a more effective pruritus-removing or therapeutic agent is desired. Further, the compound of the formula [1] is an anti-cataract agent, a prophylactic / therapeutic agent for menopausal disorders, and a cosmetic having a skin-beautifying effect (Japanese Patent Publication No. 2-44478).
No.), an anti-inflammatory agent (Japanese Patent Publication No. 1-207004), an anti-ulcer agent (JP-A No. 63-270626), an agent for preventing / treating ischemic organ injury (JP-A No. 2-111722), a bath agent (JP-A No. Applications such as No. 5-286848) are known.

[0004]

Means for Solving the Problems As a result of repeated investigations on the action of the compound [1], the present inventors have found that pruritus of the skin, which is often seen in diabetes and liver damage, and senile pruritus, which is common in the elderly, It was found that the application of this compound locally at a constant concentration is extremely effective, leading to the establishment of the present invention.

The present invention provides the following formula [1]:

[0006]

[Chemical 3] (Wherein R ₁ and R ₂ are the same or different and each independently represent a hydrogen atom or a methyl group), and a phosphodiester compound represented by the formula: It is a topical antipruritic or therapeutic agent which is contained at a concentration of 5 (w / w)% so that it can be contacted.

The present compound represented by the above formula, whether it is a free compound or a pharmacologically acceptable salt thereof, can be appropriately used for the purpose of the present invention. Examples of the salt include alkali metal salts such as sodium salt and potassium salt, and alkaline earth metal salts such as calcium salt and magnesium salt. These may be contained alone or in an appropriate combination of two or more if necessary.

The pruritus-removing or therapeutic agent of the present invention is preferably used in the form of an ointment or an aqueous agent. The aqueous agent is preferably a spray agent. For the preparation of these formulations, commonly used excipients, binders, thickeners, dispersants, reabsorption promoters, buffers, surfactants, preservatives, isotonic agents, stabilizers and pH are used. Various additives such as regulators may be used as appropriate.

The compound [1] or a salt thereof is preferably contained in the pruritus-removing agent or therapeutic agent so that it can be brought into contact with the pruritus at a concentration of 0.01 to 5 (w / w)%. If the concentration is less than the above range, the effect is insufficient, and even if the concentration exceeds the range, the effect does not change, and it is not practical.

Compound to be contained in various dosage forms [1]
The concentration of the salt is 0.01 to 5 (w / w)% in the case of ointment or cream, preferably 0.05.
2 to 2 (w / w)%, or 0.01 to 5 (w / w)% as an aqueous spray agent, preferably 0.05 to 2
(W / w)% is good.

The formulation of the present invention may appropriately contain an antihistamine agent, menthol, camphor, etc. or another type of medicinal component as long as the object of the present invention is not impaired. Hereinafter, the present invention will be described in more detail with reference to examples.

[Examples] Formulation Example 1 Ointment L-ascorbic acid, DL-α-tocopherol phosphate diester potassium 1.0 g Hydrophilic ointment total amount 100 g The above ingredients are mixed to obtain an ointment.

Formulation Example 2 Gelator L-ascorbic acid, DL-α-tocopherol phosphate diester potassium 0.5 g 1-menthol 0.5 g carbopol 1.0 g triethanolamine appropriate amount ethanol 30 ml Sterile purified water was added. Total volume adjusted to 100 ml pH 7.0

Formulation Example 3 Aqueous agent L-ascorbic acid, DL-α-tocopherol phosphate diester potassium 0.5 g glycerin 1.0 g propylene glycol 1.5 g ethanol 30 ml Sterile purified water is added to make a total volume of 100 ml.

Example 1 A 55-year-old man with eczema accompanied by itching on the abdomen and back due to liver damage was applied with the preparation of Example 1 for 2 weeks, and the eczema as well as the itch was mostly cured.

Example 2 A boy (58 years old) who always drinks sake (two sakes) in winter It was possible to get an itch and sleep well by applying the formulation of Example 3 when he had itch on his knee shin. However, there was no effect when the same formulation without the main component was applied.

Example 3 When the formulation of Example 1 was topically applied to a person who was bitten by a mosquito, itching was removed and swelling was also removed.

[0018]

INDUSTRIAL APPLICABILITY According to the present invention, there is provided a topical pruritus-removing agent or therapeutic agent which is highly effective against pruritus due to various causes.

[Procedure amendment]

[Submission date] April 3, 1995

[Procedure Amendment 1]

[Document name to be amended] Statement

[Name of item to be corrected] 0003

[Correction method] Change

[Correction content]

[0003]

2. Description of the Related Art Conventionally, ammonia water, menthol, camphor, etc. have been used for insect bites, and antihistamines or steroids have been used for the prevention of itch in urticaria. However, since these antipruritic effects are temporary, in many cases, it is necessary not only to continuously use them, but also for steroids, long-term administration requires caution due to side effect problems. Therefore, a more effective pruritus-removing or therapeutic agent is desired. Further, the compound of the formula [1] is an anti-cataract agent, a prophylactic / therapeutic agent for menopausal disorders, and a cosmetic having a skin-beautifying effect (Japanese Patent Publication No. 2-44478).
No.), anti-inflammatory agents (Kokoku 1-270 4 4 No.), an antiulcer agent (JP-63-270626), ischemic organ failure prophylactic and therapeutic agent (JP-A-2-111722), bath agents ( Applications such as JP-A-5-286848) are known.

Claims (4)

[Claims] 1. The following formula [1]: (Wherein R ₁ and R ₂ are the same or different and each independently represent a hydrogen atom or a methyl group), and a phosphodiester compound represented by the formula: A topical pruritus-removing or therapeutic agent, which is contained at a concentration of 5 (w / w)% so as to be contacted. 2. The pruritus-removing or therapeutic agent according to claim 1, which is in the form of an ointment. 3. The pruritus-removing or therapeutic agent according to claim 1, which is in the form of an aqueous liquid preparation. 4. The antipruritic or therapeutic agent according to claim 3, wherein the aqueous liquid agent is a spray agent.